CN1546016A

CN1546016A - Nanometer preparation of natural vitamin E and its preparation

Info

Publication number: CN1546016A
Application number: CNA2003101065185A
Authority: CN
Inventors: 强夏; 夏强; 顾宁; 马全红; 王以武
Original assignee: Southeast University
Current assignee: Southeast University
Priority date: 2003-12-04
Filing date: 2003-12-04
Publication date: 2004-11-17
Anticipated expiration: 2023-12-04
Also published as: CN1278682C

Abstract

The invention provides a natural vitamin E nano preparation and process for preparing it, wherein the ratio of grease material to emulsifying agent is 20:1 - 1:5, and the preparation process comprises mixing, heating, melting, charging natural vitamin E into the liquid oil phase, stirring to mix homogeneously, and carrying out emulsifying treatment.

Description

Natural Vitamin E nanometer formulation and preparation method thereof

Technical field

The present invention is the preparation method of a kind of Nano medication and cosmetic material, particularly a kind of natural Vitamin E nanometer formulation and preparation method thereof.

Background technology

Vitamin E is a kind of fat-soluble antioxidant, can suppress the generation of peroxide to the destruction and the removing free radical of free radical resisting in human body, participates in the multiple metabolic process of body.Vitamin E can strengthen the blood flow of capillary of skin, increases the resistance of blood vessel to cold, keeps the normal permeability of blood capillary, the atrophy and the degeneration of delaying skin and some organs.Vitamin E claims tocopherol again, can influence human reproductive function, can prepare natural product at present.Skin moistening, protectiving ultraviolet damage are arranged in the medicine for external use and slow down effects such as pigment or lipofuscin deposition.Some derivant of vitamin E also can be used as blood pressure lowering, blood fat reducing, prevention platelet aggregation and antiphlogistic new drug.

Except medicinal, vitamin E also is widely used in health product, nutrient, food additive and the cosmetics in recent years.Aspect food industry, vitamin E is again a kind of good deodorant, as add a certain amount of vitamin E in chewing gum, can eliminate the oral cavity stink.In shampoo, vitamin E also has deodorising effect.Vitamin E is the effective ingredient in the cosmetics.Vitamin E adds in the sensitive material, can significantly improve the performance of material etc.

The progress situation of relevant vitamin E is summarized as follows:

1. the antitumaous effect of vitamin E: vitamin E can prevent a series of cancers, as laryngocarcinoma, uterus carcinoma and breast carcinoma etc.One of Britain studies show that can produce in some physiological process of body cell have potential wasting free radical, can be neutralized by vitamin E; Vitamin E can excitating organism immunocompetence, kill the ameboid cell of new generation; Thereby vitamin E can also reach preventive effect for the cell of normal type with some malignant cell reverse.

2. vitamin E can prevent senile disease.U.S. ophthalmologist oculist finds that vitamin A easily is broken down into a kind of " age pigment "---lipofuscin that disturbs vision, makes old people's visual deterioration.And vitamin E has antioxidation, can effectively protect vitamin A to avoid oxidation and destroy, and helps and prevents senile retinal degeneration, protects and improve old people's vision, reduces and suffers from cataractous chance.U.S. geriatric nutrition researcher finds that vitamin E can obviously improve old people's immunologic function, strengthens resist the disease and infects and anti-tumor capacity.

3. vitamin E can prevent gynaecological disease.Medical research thinks that cystic cyclomastopathy and endocrine dysfunction are closely related.Vitamin E can reduce the possibility of suffering from breast carcinoma, and tuberosity or cyst are disappeared.

4. vitamin E can prevent other diseases.External science researcher thinks: gastric ulcer patient gastric mucosa fragility, and relevant with the lipid peroxidation disorder, and vitamin E is a powerful antioxidant, can make pain relief, weight increase, ulcer scar scarization.China's medical circle finds that also Keshan disease patient has the constitutional hepar damnification, makes liver T451 take off single iodine enzyme and reduces.And vitamin E can prevent the formation of lipid peroxide, and membrane structure is had protective effect, can strengthen the activity that liver cell T451 takes off single iodine enzyme, improves the oxidative metabolism of cardiac muscle, thereby has reduced the sickness rate of Keshan disease.Vitamin E can stop ldl cholesterol oxidation, thereby avoids coronary atherosclerosis, impels vasodilation, prevents cardiovascular disease.

5. vitamin E is widely used in food additive, and it and ascorbic synergism can more effectively stop the nitrite in the foods such as bacon, sausage, Petaso to form the carcinogen nitrosamine under one's belt.

In addition, vitamin E all produces effect to common diseases such as control sural spasm, poliosis, epistaxis, bleeding hemorrhoids, chilblain.

In sum, vitamin E is a kind of purposes medicine and daily chemical industry raw material very widely.

At present, the form of medication of vitamin E mainly concentrates on oral liquid, injection, soft gelatin capsule etc., and exterior-applied formulation mainly contains cream, ointment etc.Form of medication is generally acknowledged by research worker the importance of medicine performance drug effect.And when using above-mentioned dosage form as the vitamin E of fat-soluble medicine, the same with other fat-soluble medicines, in various degree have that bioavailability is low, the deficiency of absorption difference.

The development Nano medication then might overcome above problem.Can significantly improve its bioavailability after the medicament nanoization.The size and the particle size distribution of control medicament nano granule can control drug release speed, improve efficacy of drugs and effective rate of utilization.

At present, in the Nano medication research field, the screening of pharmaceutical carrier and optimization of preparation have become research emphasis.Present carrier comprises polymer nanoparticle, nanoemulsions, liposome, nano suspending liquid, solid lipid nanoparticle, nano structured lipid carrier etc.Then both then are the novel liposoluble medicament nano carriers that grows up from the nineties in last century.

Summary of the invention

Technical problem: the present invention is directed to some problems that existing Vitamin E preparation aspect exists, various informative natural Vitamin E nanometer formulation of a kind of drug loading height, formulation products and preparation method thereof is provided.

Technical scheme: the vitamin E nano preparation preparation method as follows:

1. distinguish weighing matrix material and emulsifying agent, both mass ratioes, i.e. matrix material: emulsifying agent is 20: 1～1: 5; Matrix material and emulsifier post-heating to design temperature T, promptly T=60-80 degree centigrade, are obtained liquid oil phase after the fusion;

2. natural Vitamin E is joined in the liquid oil phase, mix the clarification system;

3. above-mentioned clarification system is joined in the water with design temperature T uniform temp, behind the mix homogeneously, carried out emulsifying 1-60 minute, obtain the natural Vitamin E nanometer formulation.Can be dissolved with the water soluble surfactant active in the water.

4. the aqueous dispersion that obtains in the step 3 can further carry out lyophilization and handles and to obtain lyophilized powder.

Matrix material is one or more the mixture in the above fatty acid of 12 carbochains, vegetable oil, the fatty glyceride.

Emulsifying agent is a nonionic surfactant, comprises one or more the mixture in department class, tween, polyoxyl stearate S-40, poloxamer F-68, the fabaceous lecithin etc.

Emulsifying comprises the emulsifying that one or more carried out that adopts in mechanical agitation, magnetic agitation, high cut disperse emulsification, high pressure homogenize emulsifying, the ultrasonic emulsification etc.

Described nanometer formulation comprises matrix material and vitamin E, and its form specifically is divided into: matrix material is to be the material of liquid phase under a kind of room temperature, and final prepared nanometer formulation is called nanoemulsions; Matrix material is to be the material of solid phase under a kind of room temperature, and final prepared nanometer formulation is called solid lipid nanoparticle; Matrix material is multiple mixtures of material, and final prepared nanometer formulation is called nano structured lipid carrier.

Beneficial effect: adopt method of the present invention to prepare the nanometer formulation of vitamin E, compare, have a lot of usefulness with existing vitamin E dosage form:

1 nanometer formulation product form is various: matrix material is to be the material of liquid phase under a kind of room temperature, and final prepared nanometer formulation is called nanoemulsions; Matrix material is to be the material of solid phase under a kind of room temperature, and final prepared nanometer formulation is called solid lipid nanoparticle; Matrix material is multiple mixtures of material, and final prepared nanometer formulation is called nano structured lipid carrier.

2 lipid concentrations can bring up to 25%, and drug loading can bring up to 20%.

The particle size range that is loaded with the nanoparticle of vitamin E in 3 nanometer formulations is the 100-200 nanometer.

4 preparation process are simple and convenient, and repeatability is high.

5 select water as medium the biocompatibility of the medicine that makes to be greatly improved.

The prepared vitamin E nano preparation of 6 moisture retention test shows all has the good moisture preserving effect.

7 is cryoprotective agent with mannitol, the aqueous dispersion that obtains can be prepared into lyophilized powder, and convenient transportation is preserved and used.

Description of drawings

Fig. 1 is the schematic flow sheet of preparation process of the present invention.

The specific embodiment

Embodiment one:

1, weighing 0.5 gram stearic acid, 0.15 gram fabaceous lecithin,, be heated to 75 ℃ of mix homogeneously and obtain liquid oil phase;

2, weighing 0.1 gram natural Vitamin E joins in the liquid oil phase, mix the clarification system;

3, weighing 2.0 gram S-40 are dissolved in 100 ml waters, are heated to 75 ℃;

4, resulting clarification system in the step 2 is joined in 100 milliliters of 75 ℃ of water, behind the mix homogeneously, do not adopt magnetic agitation equipment and ultrasonic processing equipment to carry out emulsifying 30 minutes and 10 minutes;

5. be cooled to room temperature and promptly obtain the solid lipid nanoparticle of natural Vitamin E.

Embodiment two:

Weighing 6 gram stearic acid, 4 gram soybean oils, 1.5 gram fabaceous lecithins,, be heated to 75 ℃ of mix homogeneously and obtain liquid oil phase;

2. weighing 1.0 gram natural Vitamin E join in the liquid oil phase, mix the clarification system;

3. weighing 10 gram S-40 are dissolved in 1000 ml waters, are heated to 75 ℃;

4. resulting clarification system in the step 2 is joined in 1000 milliliters of 75 ℃ of water, behind the mix homogeneously, adopt high pressure homogenizer to carry out emulsifying 3 minutes;

5. be cooled to room temperature and promptly obtain the nano structured lipid carrier of natural Vitamin E.

Embodiment three:

1. weighing 5 gram soybean oils, 0.75 gram fabaceous lecithin are heated to 60 ℃ of mix homogeneously and obtain liquid oil phase;

2. weighing 0.5 gram natural Vitamin E joins in the liquid oil phase, mix the clarification system;

3. 500 ml waters are heated to 60 ℃;

4. resulting clarification system in the step 2 is joined in 500 milliliters of 75 ℃ of water, behind the mix homogeneously, adopt high pressure homogenizer to carry out emulsifying 2 minutes;

5. be cooled to room temperature and promptly obtain the nanoemulsions of natural Vitamin E.

Claims

1, a kind of natural Vitamin E nanometer formulation and preparation method thereof is characterized in that preparation flow is:

(1), respectively weighing matrix material and emulsifying agent, both mass ratioes, i.e. matrix material: emulsifying agent is 20: 1～1: 5, and matrix material and emulsifier post-heating to design temperature T, promptly T=60-80 degree centigrade, are obtained liquid oil phase after the fusion;

(2), natural Vitamin E is joined in the liquid oil phase, mix the clarification system;

(3), above-mentioned clarification system is joined in the water with design temperature T uniform temp, behind the mix homogeneously, carried out emulsifying 5-60 minute, obtain the natural Vitamin E nanometer formulation.

2, natural Vitamin E nanometer formulation according to claim 1 and preparation method thereof is characterized in that described matrix material is one or more the mixture in the above fatty acid of 12 carbochains, vegetable oil, the fatty glyceride.

3, natural Vitamin E nanometer formulation according to claim 1 and preparation method thereof, it is characterized in that described emulsifying agent is a nonionic surfactant, comprise one or more the mixture in department class, tween, polyoxyl stearate S-40, poloxamer F-68, the fabaceous lecithin etc.

4, natural Vitamin E nanometer formulation according to claim 1 and preparation method thereof is characterized in that described emulsifying comprises the emulsifying that one or more carried out that adopts in mechanical agitation, magnetic agitation, high cut disperse emulsification, high pressure homogenize emulsifying, the ultrasonic emulsification etc.

5, preparation natural Vitamin E nanometer formulation according to claim 1 and preparation method thereof is characterized in that can being dissolved with the water soluble surfactant active in the described water.

6, preparation natural Vitamin E nanometer formulation according to claim 1 and preparation method thereof is characterized in that the aqueous dispersion that obtains can further carry out the lyophilization processing and obtain lyophilized powder in step 3.

7, a kind of as claim 1 or 2 or 3 or 4 or 5 prepared natural Vitamin E nanometer formulations, it is characterized in that described nanometer formulation comprises matrix material and vitamin E, its form specifically is divided into: matrix material is to be the material of liquid phase under a kind of room temperature, and final prepared nanometer formulation is called nanoemulsions; Matrix material is to be the material of solid phase under a kind of room temperature, and final prepared nanometer formulation is called solid lipid nanoparticle; Matrix material is multiple mixtures of material, and final prepared nanometer formulation is called nano structured lipid carrier.